Journal of medicinal chemistry

Biological evaluation of bishydroxymethyl-substituted cage dimeric 1, 4-dihydropyridines as a novel class of p-glycoprotein modulating agents in cancer cells

M Richter, J Molnár, A Hilgeroth

Index: Richter, Martin; Molnar, Josef; Hilgeroth, Andreas Journal of Medicinal Chemistry, 2006 , vol. 49, # 9 p. 2838 - 2840

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Citation Number: 22

Abstract

A series of N-substituted cage dimeric 1, 4-dihydropyridines 3a-e was evaluated as inhibitors of membrane efflux pump P-glycoprotein (P-gp) in multidrug resistant (mdr) cancer cells. Structure-activity relationships (SAR) and cytotoxic properties are discussed. Effective concentrations for overcoming mdr have been demonstrated in competition studies with the P-gp substrate epirubicin.